182439-41-4

Basic information

• Product Name: N-(piperidin-4-yl)-4'-(trifluoromethyl)-[1,1'-biphenyl]-2-carboxamide
• Synonyms: N-(piperidin-4-yl)-4'-(trifluoromethyl)-[1,1'-biphenyl]-2-carboxamide;N-4-Piperidinyl-4'-(trifluoromethyl)-[1,1'-biphenyl]-2-carboxamide
• CAS NO: 182439-41-4
• Molecular Formula: C₁₉H₁₉F₃N₂O
• Molecular Weight: 348.3621696
• Mol File: 182439-41-4.mol
• Article Data: 5

Chemical Properties

• Appearance: /
• CAS DataBase Reference: N-(piperidin-4-yl)-4'-(trifluoromethyl)-[1,1'-biphenyl]-2-carboxamide(CAS DataBase Reference)
• NIST Chemistry Reference: N-(piperidin-4-yl)-4'-(trifluoromethyl)-[1,1'-biphenyl]-2-carboxamide(182439-41-4)
• EPA Substance Registry System: N-(piperidin-4-yl)-4'-(trifluoromethyl)-[1,1'-biphenyl]-2-carboxamide(182439-41-4)

Safety Data

• Hazardous Substances Data: 182439-41-4(Hazardous Substances Data)

Usage

Uses

N-(Piperidin-4-yl)-4''-(trifluoromethyl)-biphenyl-2-carboxamide is a reagent used in the preparation of lomitapide mesylate crystal forms. Lomitapide mesylate is a microsomal triglyceride transfer protein inhibitor which can lower the level of low density lipoprotein cholesterol in plasma. Lomitapide (L469435) metabolite.

Upstream product

• 87120-72-7 1-(tert-butoxycarbonyl)-4-aminopiperidine 
• 128796-39-4 4-trifluoromethylphenylboronic acid 
• 88-67-5 2-Iodobenzoic acid 
• 50541-93-0 4-amino-1-benzylpiperidine 
• 84392-17-6 4'-(trifluoromethyl)-2-biphenylcarboxylic acid 
• 182439-40-3 N-(1-benzylpiperidin-4-yl)-4'-(trifluoromethyl)-[1,1'-biphenyl]-2-carboxamide 

Downstream Products

• 594844-53-8 [4-(4'-trifluoromethylbiphenyl-2-carbonylamino)piperidin-1-yl]acetic acid ethyl ester 
• 202914-84-9 N-(2,2,2-trifluoroethyl)-9-[4-[4-[[[4’-(trifluoromethyl)[1,1‘-biphenyl]-2-yl]carbonyl]amino]-1-piperidinyl]butyl]-9H-fluorene-9-carboxamide methanesulfonate 
• 182431-12-5 9-[4-[4-[[[4'-(trifluoromethyl)[1,1'-biphenyl]-2-yl]carbonyl]amino]-1-piperidinyl]butyl]-N-(2,2,2-trifluoroethyl)-9H-fluorene-9-carboxamide 

Relevant articles and documents

Synthetic method of lomitapide-D8

The invention provides a synthetic method of lomitapide-D8. The method comprises the following steps: 1) performing a halogenation reaction on a compound 2a and hydrobromic acid to obtain a compound 2; 2) carrying out a hydrogen abstraction reaction on a compound 1 and n-butyllithium, and then adding the compound 2 to carry out a substitution reaction to prepare a compound 3; 3) performing a condensation reaction on the compound 3 and a compound 4 to obtain a compound 5; 4) performing a condensation reaction on a compound 6 and a compound 7 to obtain a compound 8; 5) removing tert-butyloxycarbonyl protection from the compound 8 by utilizing trifluoroacetic acid to obtain a compound 9; and 6) subjecting the compound 5 and the compound 9 to a substitution reaction to obtain the lomitapide-D8. Through the method, deuterated tetrahydrofuran with relatively low price is used as a raw material to synthesize the deuterated 1,4-dibromobutane-D8 for the first time, the deuterated lomitapide-D8is successfully synthesized, and a conventional synthesis route is changed, so that deuterated atoms which are difficult to obtain reach the maximum atom economic effect.

PROCESS FOR THE PREPARATION OF LOMITAPIDE

The present invention relates to a process for preparing Lomitapide or its pharmaceutically acceptable salt thereof having high purity with acceptable levels of impurities.

Biphenyl derivatives, production thereof and uses as medicines

The present invention relates to biphenyl derivatives of general formula wherein Rato Rgand n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyceride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.